KR890006593A - Armatase Inhibition 4 (5) -imidazole - Google Patents

Armatase Inhibition 4 (5) -imidazole Download PDF

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KR890006593A
KR890006593A KR1019880013196A KR880013196A KR890006593A KR 890006593 A KR890006593 A KR 890006593A KR 1019880013196 A KR1019880013196 A KR 1019880013196A KR 880013196 A KR880013196 A KR 880013196A KR 890006593 A KR890006593 A KR 890006593A
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imidazole
bis
benzyl
propyl
propen
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요하네스 카잘라이넨 아르토
베익코 말티 칸가스 로리
오이바 안테로 쿠르켈라 카우코
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하이키 오얀페래, 하칸 코트카
파르모스-이티마오이
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    • C07—ORGANIC CHEMISTRY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine

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Abstract

내용 없음No content

Description

아르마타제 억제4(5)-이미다졸Armatase Inhibition 4 (5) -imidazole

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (12)

하기 일반식(Ⅰ)의 치환된 이미다졸 또는 제약악적으로 허용가능한 이들의 무-독성 산 부가염:Substituted imidazoles of formula (I) or pharmaceutically acceptable non-toxic acid addition salts thereof: 상기식에서 R1, R2, R1' 및 R2'는 같거나 다를 수 있는 것을 H, CH3, C2H5, OCH3, OH, CH2OH, NH2, 또는 할로겐이며; R'는 H 또는(여기에서 R3은 H, CH3또는 할로겐임)이며; R4는 H이며 R5는 H 또는 OH이며 R6는 H 또는 OH이거나 R5와 R6중 하나는 H이며 다른 하나는 R4와 함께 결합을 형성하며 X와 Y는 같거나 다를 수 있는 것을 결합, 직쇄 C1-2-알킬 또는 상응하는 알케닐이다.Wherein R 1 , R 2 , R 1 ′ and R 2 ′ may be the same or different H, CH 3 , C 2 H 5 , OCH 3 , OH, CH 2 OH, NH 2 , or halogen; R 'is H or Wherein R 3 is H, CH 3 or halogen; R 4 is H, R 5 is H or OH, R 6 is H or OH, or one of R 5 and R 6 is H and the other together with R 4 form a bond and X and Y may be the same or different a bond, a straight-chain C 1 - 2 - alkyl or the corresponding alkenyl. 하기 일반구조식의 치환된 이미다졸 또는 제약학적으로 허용 가능한 이들의 무-독성 산 부가염.Substituted imidazoles of the following general formula or pharmaceutically acceptable non-toxic acid addition salts thereof. 상기식에서 R1, R2, 와 R1' 및 R2'는 같거나 다를 수 있는 것으로 H, CH3, C2H5, OCH3, OH, CH2OH, NH2, 또는 할로겐이며; R'는 H 또는(여기에서 R3은 H, CH3또는 할로겐임)이며; R4는 H이며 R5는 H이거나 R4와 R5는 함께 결합을 형성한다.Wherein R 1 , R 2 , and R 1 ′ and R 2 ′ may be the same or different and are H, CH 3 , C 2 H 5 , OCH 3 , OH, CH 2 OH, NH 2 , or halogen; R 'is H or Wherein R 3 is H, CH 3 or halogen; R 4 is H and R 5 is H or R 4 and R 5 together form a bond. 제2항에 있어서, R4와 R4가 모두 H인 치환된 이미다졸.3. The substituted imidazole of claim 2, wherein R 4 and R 4 are both H. 제2항에 있어서, R4와 R4가 함께 결합을 형성하는 치환된 이미다졸.The substituted imidazole of claim 2, wherein R 4 and R 4 together form a bond. 제2항 내지 제4항 중 어느한 항에 있어서, R1, R2, R1', R2' 및 중 적어도 한개의 H가 아니며 치환체 R1, R2, R1' 및 R2'중 한개 이상의 페닐기의 3,5,3' 또는 5'위치에 있는 치환된 이미다졸.The compound according to any one of claims 2 to 4, wherein at least one of R 1 , R 2 , R 1 ′, R 2 ′, and H is not selected from the substituents R 1 , R 2 , R 1 ′, and R 2 ′. Substituted imidazole at the 3,5,3 'or 5' position of one or more phenyl groups. 제5항에 있어서, R2및 R2'는 H 이며 R1및 R1'은 둘다 수소가 아니며 둘다 페닐기의 메타 위치에 있는 치환된 이미다졸.The substituted imidazole of claim 5, wherein R 2 and R 2 ′ are H and R 1 and R 1 ′ are both not hydrogen and both are in the meta position of the phenyl group. 제2항 내지 제6항중 어느 한항에 있어서, R'가 H인 치환된 이미다.The substituted imine of claim 2, wherein R ′ is H. 8. 제2항 내지 제6항중 어느 한항에 있어서, R'가(여기에서 R3은 H,CH3또는 할로겐임)인 치환된 이미다졸.The compound of any one of claims 2 to 6, wherein R 'is Wherein R 3 is H, CH 3 or halogen. 제8항에 있어서, R3이 H인 치환된 이미다졸.The substituted imidazole of claim 8, wherein R 3 is H. 10. 제1항에 있어서, 4-[5-(2,6-디메틸페닐)-3-히드록시-3-(2,6-디메틸페닐-에틸)펜틸]-1H-이미다졸, 4-[3,3-비스(4-클로로페닐)-3-히드록시프로필)-1H-이미다졸, 4-[3,3-디페닐-3-히드록시프로필)-1H-이미다졸, 4-(3,3-디페닐프로펜-2-일)-1H-이미다졸, 4-(3,3-디페닐프로필)-1H-이미다졸, 4-[3,3-비스(2-메틸페닐)-3-히드록시프로필]-1H-이미다졸, 4-[3,3-비스(4-클로로페닐)프로펜-2-일]1H-이미다졸, 4-[3,3-비스-(2-메틸페닐)프로펜-2-일]-1H-이미다졸, 4-[3,3-비스(2-메틸페닐)프로필]-1H-이미다졸, 1-벤질-4-(3,3-디메닐프로필)-1H-이미다졸, 1-벤질-5-(3,3-디페닐 프로필)-1H-이미다졸, 4-[3,3-비스((3-메틸페닐)프로필]-1H-이미다졸, 4-[3,3-비스-(3-메틸페닐)프로펜-2-일]-1H-이미다졸, 1-(4-클로로벤질)-4-(3,3-디페닐프로필)-1H-이미다졸, 1-(4-클로로벤질)-5-(3.3-디페닐프로필)-1H-이미다졸, 4-[5-(2,6-디메틸페닐)-3-(2,6-디메틸페닐에틸)-펜틸]-1H-이미다졸, 4-[3,3-비스(3,5-디메틸페닐)프로필]-1H-이미다졸, 4-[3,3-비스(3-메톡시페닐)프로필]-1H-이미다졸, 4-[3,3-비스(2,3-디메틸페닐)프로필]-1H-이미다졸, 1-벤질-5-[3,3-비스(3-메톡시페닐)프로필]-1H-이미다졸, 1-벤질-5-[3,3-비스(3-메턱시페닐 프로펜-2-일]-1H-이미다졸, 4-[3,3-비스(3,5-디메틸페닐)프로필]-1H-이미다졸, 4-[3,3-비스(4-메톡시페닐)프로필-1H-이미다졸, 4-[3,3-비스(3-플루오로페닐)프로필]-1H-이미다졸,1-벤질 -5[3,3-비스(4-클로로페닐)3-히드록시프로필]-1H-이미다졸, 1-벤질-5-[3,3-1ㅣ스(4-클로로페닐)프로펜-2-일]-1H-이미다졸, 4-[3-(4-클로로페닐)-3-히드록시-3-페닐프로필]-1H-이미다졸, 4-[3,3[-비스(3-메틸페닐)-3-히드록시프로필-1H-이미다졸, 4-[3,3-비스(3-플루오로페닐)ㅡ프로펜-2-일]-1H-이미다졸, 1-벤질-5-[5-(2,6-디메틸페닐)-3-히드록시-3-(2,6-디메틸페닐에틸)-펜틸]-1H-이미다졸, 1-벤질-5-[3,3-비스(3,5-디메틸페닐)-3-히이록시프로필]-1H-이미다졸, 1-벤질-5-[3,3-비스(3,5-디메틸페닐)프로펜-2-일]-1H-이미다졸, 1-벤질-5-[3,3-비스(2-메톡시페닐)프로펜-2-일]-1H-이미다졸, 1-벤질-5[3,3-비스(4-메톡시페닐)프로펜-2-일]-1H-이미다졸, 1-벤질-5-[3,3-비스(2,3-디메틸페닐)프로펜-2-일]-1H-이미다졸, 1-벤질-5-[3,3-비스(2-메틸페닐)프로펜-2-일]-1H-이미다졸, 1-벤질-5-[3,3-비스)(3-메틸페닐)프로펜-2-일]-1H-이미다졸, 4-[3,3-비스(2-메톡시페닐)프로필]-1H-이미다졸, 4-[3,3-비스(4-메톡시페닐)프로필]-1H-이미다졸, 1-벤질-5-[3,3-비스(4-메틸페닐)프로펜-2-일]-1H-이미다졸 또는 1-벤질-5-(3,3-디페닐프로펜-2-일]-1H-이미다졸 또는 제약적으로 허용가능한 이들의 무독성 산부가염인 화합물.A compound according to claim 1, wherein 4- [5- (2,6-dimethylphenyl) -3-hydroxy-3- (2,6-dimethylphenyl-ethyl) pentyl] -1 H-imidazole, 4- [3, 3-bis (4-chlorophenyl) -3-hydroxypropyl) -1H-imidazole, 4- [3,3-diphenyl-3-hydroxypropyl) -1H-imidazole, 4- (3,3 -Diphenylpropen-2-yl) -1H-imidazole, 4- (3,3-diphenylpropyl) -1H-imidazole, 4- [3,3-bis (2-methylphenyl) -3-hydrate Roxypropyl] -1H-imidazole, 4- [3,3-bis (4-chlorophenyl) propen-2-yl] 1H-imidazole, 4- [3,3-bis- (2-methylphenyl) prop Phen-2-yl] -1H-imidazole, 4- [3,3-bis (2-methylphenyl) propyl] -1H-imidazole, 1-benzyl-4- (3,3-dimenylpropyl) -1H -Imidazole, 1-benzyl-5- (3,3-diphenyl propyl) -1H-imidazole, 4- [3,3-bis ((3-methylphenyl) propyl] -1H-imidazole, 4- [ 3,3-bis- (3-methylphenyl) propen-2-yl] -1H-imidazole, 1- (4-chlorobenzyl) -4- (3,3-diphenylpropyl) -1H-imidazole, 1- (4-chlorobenzyl) -5- (3.3-diphenylpropyl) -1H-imidazole, 4- [5- (2,6-dimethylphenyl) -3- (2,6- Dimethylphenylethyl) -pentyl] -1 H-imidazole, 4- [3,3-bis (3,5-dimethylphenyl) propyl] -1 H-imidazole, 4- [3,3-bis (3-methoxy Phenyl) propyl] -1H-imidazole, 4- [3,3-bis (2,3-dimethylphenyl) propyl] -1H-imidazole, 1-benzyl-5- [3,3-bis (3-meth Methoxyphenyl) propyl] -1H-imidazole, 1-benzyl-5- [3,3-bis (3-methoxyphenyl propen-2-yl] -1H-imidazole, 4- [3,3-bis (3,5-dimethylphenyl) propyl] -1H-imidazole, 4- [3,3-bis (4-methoxyphenyl) propyl-1H-imidazole, 4- [3,3-bis (3-fluoro Rophenyl) propyl] -1H-imidazole, 1-benzyl-5 [3,3-bis (4-chlorophenyl) 3-hydroxypropyl] -1H-imidazole, 1-benzyl-5- [3,3 -1s (4-chlorophenyl) propen-2-yl] -1H-imidazole, 4- [3- (4-chlorophenyl) -3-hydroxy-3-phenylpropyl] -1H-imidazole, 4- [3,3 [-bis (3-methylphenyl) -3-hydroxypropyl-1H-imidazole, 4- [3,3-bis (3-fluorophenyl) -propen-2-yl]- 1H-imidazole, 1-benzyl-5- [5- (2,6-dimethylphenyl) -3-hydroxy-3- (2,6-di Tylphenylethyl) -pentyl] -1 H-imidazole, 1-benzyl-5- [3,3-bis (3,5-dimethylphenyl) -3-hydroxypropyl] -1 H-imidazole, 1-benzyl- 5- [3,3-bis (3,5-dimethylphenyl) propen-2-yl] -1H-imidazole, 1-benzyl-5- [3,3-bis (2-methoxyphenyl) propene -2-yl] -1 H-imidazole, 1-benzyl-5 [3,3-bis (4-methoxyphenyl) propen-2-yl] -1 H-imidazole, 1-benzyl-5- [3 , 3-bis (2,3-dimethylphenyl) propen-2-yl] -1H-imidazole, 1-benzyl-5- [3,3-bis (2-methylphenyl) propen-2-yl]- 1H-imidazole, 1-benzyl-5- [3,3-bis) (3-methylphenyl) propen-2-yl] -1H-imidazole, 4- [3,3-bis (2-methoxyphenyl ) Propyl] -1H-imidazole, 4- [3,3-bis (4-methoxyphenyl) propyl] -1H-imidazole, 1-benzyl-5- [3,3-bis (4-methylphenyl) prop Phen-2-yl] -1H-imidazole or 1-benzyl-5- (3,3-diphenylpropen-2-yl] -1H-imidazole or a pharmaceutically acceptable non-toxic acid addition salt thereof. 제1항 내지 제10항중 어느 한항에 청구된 치환된 이미다졸 및 제약적으로 허용가능한 담체를 포함하는 제약적인 조성물.A pharmaceutical composition comprising the substituted imidazole claimed in any one of claims 1 to 10 and a pharmaceutically acceptable carrier. 아로마타지제 억제 제로서 사용하기 위한 제1항 내지 11항중 어느 한항에 따르는 이미다졸 유도체 또는 무독성 산부가염.An imidazole derivative or non-toxic acid addition salt according to any one of claims 1 to 11 for use as an aromatase inhibitor. ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is to be disclosed based on the initial application.
KR1019880013196A 1987-10-09 1988-10-08 Armatase Inhibition 4 (5) -imidazole KR890006593A (en)

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GB8723715 1987-10-09
GB8723715A GB2210875B (en) 1987-10-09 1987-10-09 Aromatase inhibiting 4(5)-imidazoles

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FI884497A0 (en) 1988-09-30
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JPH01132568A (en) 1989-05-25
IL87969A0 (en) 1989-03-31
NO172048C (en) 1993-06-02
AU615482B2 (en) 1991-10-03
EP0311447B1 (en) 1992-08-26
RU1819263C (en) 1993-05-30
NO172048B (en) 1993-02-22
US5098923A (en) 1992-03-24
UA13218A (en) 1997-02-28
DE3874073D1 (en) 1992-10-01
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DD282912A5 (en) 1990-09-26
IL87969A (en) 1993-04-04
NO884473D0 (en) 1988-10-07
PT88717B (en) 1992-12-31
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EP0311447A1 (en) 1989-04-12
GB2210875B (en) 1991-05-29
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CA1329616C (en) 1994-05-17
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AU2349088A (en) 1989-04-13
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HU201024B (en) 1990-09-28
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DE3874073T2 (en) 1993-01-21

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